Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 20, Issue 7, Pages 2344-2349Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.01.132
Keywords
GSK3beta; Tau phosphorylation; Amide hydrolysis; Metabolic stability; Kinase
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From potent and selective inhibitors of GSK3 beta displaying CYP1A2 inhibition and poor PK properties, mostly linked to metabolic instability and in vivo hydrolysis of the amide bond, we were able to obtain safe and orally available inhibitors with good half lives. (C) 2010 Elsevier Ltd. All rights reserved.
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